Table 2.
Inhibitory activity of compounds 2a–d, 2h, 2i–n, and 2q, and IC50 (μM) of compounds 2a–c, 2q against protein kinases.
| N | % Inhibition * | IC50 (μM) | |||||||
|---|---|---|---|---|---|---|---|---|---|
| NPM1- ALK |
ALK | EGFR [L858R] [T790] |
CRAF [Y340D] [Y341D] |
JAK2 | JAK3 | CRAF [Y340D] [Y341D] | JAK3 | NPM1- ALK |
|
| 2a | 87 | 84 | 82 | 93 | 81 | 96 | 6.57 | 0.36 | 0.54 |
| 2b | 90 | 86 | 84 | 92 | 83 | 95 | N/A- | 0.38 | 0.25 |
| 2c | 75 | 77 | 88 | 93 | 76 | 95 | 0.78 | 0.41 | - |
| 2d | 41 | 39 | 12 | 61 | 33 | 69 | - | - | - |
| 2h | 42 | 49 | 27 | 44 | 10 | 36 | - | - | - |
| 2i | 77 | 81 | 24 | 76 | 64 | 89 | - | - | - |
| 2j | 56 | 7 | 9 | 5 | 11 | 39 | - | - | - |
| 2k | 27 | 18 | −2 | 41 | 3 | 26 | - | - | - |
| 2l | 67 | 75 | 24 | 81 | 53 | 86 | - | - | - |
| 2m | 6 | −4 | 10 | 35 | 1 | 23 | - | - | - |
| 2n | 24 | 19 | 5 | 13 | 47 | 52 | - | - | - |
| 2q | 36 | 51 | 71 | 92 | 9 | 99 | 5.34 | 0.46 | - |
| sorafenib | - | - | - | - | - | - | 1.95 | 0.78 | 0.43 |
* The decrease in intensity compared to the fluorescence intensity for the native enzyme in a blank experiment without the addition of an inhibitor.